2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Somatostatin Receptor

Somatostatin Receptor

SSTRs; SSTR

Somatostatin Receptor

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Somatostatin receptors (SSTR1, 2A and B, 3, 4 and 5) belong to the G protein coupled receptor family. Somatostatin receptors are expressed in a variety of human tumors, including most tumors of neuroendocrine origin, breast tumors, certain brain tumors, renal cell tumors, lymphomas, and prostate cancer. Somatostatin triggers cytostatic and cytotoxic effects and has a general inhibitory effect on secretion mediated through its interaction with somatostatin receptors.

The SSTRs 1-4 display weak selectivity for somatostatin-14 binding, whereas SSTR5 is somatostatin-28-selective. Based on structural similarity and reactivity for octapeptide and hexapeptide somatostatin receptor analogs, SSTRs 2, 3 and SSTR5 belong to a similar somatostatin receptor subclass; SSTRs 1-4 react poorly with these analogs and belong to a separate subclass. All five somatostatin receptors are functionally coupled to inhibition of adenylyl cyclase via pertussis toxin-sensitive guanosine triphosphate (GTP)-binding proteins. mRNA for SSTRs 1-5 is widely expressed in brain and peripheral organs and displays an overlapping but characteristic pattern that is subtype-selective and tissue- and species-specific. All pituitary cell subsets express SSTR2 and SSTR5, with SSTR5 being more abundant. Individual pituitary cells coexpress multiple somatostatin receptor subtypes.

Somatostatin Receptor Isoform Specific Products:

Somatostatin Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P4100
    Cyclic SSTR agonist octreotide
    		Agonist
    Cyclic SSTR agonist octreotide is a Octreotide (HY-P0036), serving as the cyclic Somatostatin Receptor SSTR agonist.
    Cyclic SSTR agonist octreotide
  • HY-108497A
    L-803087 TFA
    		Agonist
    L-803087 TFA is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 TFA is >280-fold more selective for sst4 receptor than other somatostatin receptors. L-803087 TFA facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice.
    L-803087 TFA
  • HY-P10758
    Alkyne-βAG-TOCA
    		Agonist
    Alkyne-βAG-TOCA, an octreotide derivative, targets somatostatin receptor type 2 (SST2). Alkyne-βAG-TOCA can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    Alkyne-βAG-TOCA
  • HY-123335
    L-796,778
    		Agonist
    L-796,778 is an agonist of the hsst3 receptor. In CHO-K1 cells expressing the hsst3 receptor, L-796,778 is a partial agonist that inhibits forskolin (HY-15371)-stimulated cAMP production with an IC50 value of 18 nM.
    L-796,778
  • HY-P10741
    DOTA-EB-TATE
    		Activator
    DOTA-EB-TATE is composed of SST peptide derivative, DOTA-octreotate conjugated a common to an Evans blue analog (EB). DOTA-EB-TATE is a peptide drug conjugate (PDC) improves the pharmacokinetics of SSTR2 analogs and reduces PRRT toxicity. DOTA-EB-TATE can also be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    DOTA-EB-TATE
  • HY-RS13829
    SSTR4 Human Pre-designed siRNA Set A
    		Inhibitor

    SSTR4 Human Pre-designed siRNA Set A contains three designed siRNAs for SSTR4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    SSTR4 Human Pre-designed siRNA Set A
    SSTR4 Human Pre-designed siRNA Set A
  • HY-RS13823
    SSTR2 Human Pre-designed siRNA Set A
    		Inhibitor

    SSTR2 Human Pre-designed siRNA Set A contains three designed siRNAs for SSTR2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    SSTR2 Human Pre-designed siRNA Set A
    SSTR2 Human Pre-designed siRNA Set A
  • HY-123460
    BN-81674
    		Antagonist
    BN-81674 is a somatostatin analogue and a selective antagonist of the non-peptide human somatostatin sst3 receptor (Ki=0.92 nM). In addition, BN-81674 reversed the inhibition of cyclic AMP accumulation induced by 1 nM somatostatin through the sst3 receptor with an IC50 value of 0.84 nM. BN-81674 can be used in cancer research.
    BN-81674
  • HY-139347
    SSTR4 agonist-1
    		Agonist 99.09%
    SSTR4 agonist-1 (Compound 47) is a selective agonist for somatostatin receptor subtype 4 (SSTR4) with an EC50 of 4.7 nM. SSTR4 agonist-1 reveals a half-life > 130 minutes in human liver microsomes.
    SSTR4 agonist-1
  • HY-P1959
    Lanreotide
    		Activator
    Lanreotide (BIM 23014) is a somatostatin analogue with antineoplastic activity. Lanreotide can be used for the research of carcinoid syndrome.
    Lanreotide
  • HY-163317A
    MMC(TMZ)-TOC TFA
    MMC(TMZ)-TOC TFA has high binding affinity and selectivity for somatostatin receptor subtype-2 (SSTR2). MMC(TMZ)-TOC TFA targets delivery of TMZ to SSTR2-positive tumor cells. MMC(TMZ)-TOC TFA can be used for the research of cancer.
    MMC(TMZ)-TOC TFA
  • HY-109155A
    Paltusotine hydrochloride
    		Agonist
    Paltusotine (CRN00808) hydrochloride is an orally active, nonpeptide selective somatostatin type 2 (SST2) receptor agonist. Paltusotine hydrochloride has the potential for maintaining GH and IGF-1 levels after depot somatostatin receptor ligand therapy.Paltusotine hydrochloride can be used in research on acromegaly and neuroendocrine tumors.
    Paltusotine hydrochloride
  • HY-159825
    Branosotine
    		Agonist
    Branosotine (compound 1-1) is a potent agonist of somatostatin receptor (SSTR2), with the EC50 of ＜0.1 nM.
    Branosotine
  • HY-164040
    Zavolosotine
    		Agonist
    Zavolosotine (Compound 1) is an orally active agonist for somatostatin receptor type 5 (SST5) with EC50 <1 nM. Zavolosotine inhibits insulin and glucagon secretion, increases levels of glucagon in blood in rat model.
    Zavolosotine
  • HY-139347A
    SSTR4 agonist-1 tartrate
    		Agonist
    SSTR4 agonist-1 tartrate (Preparation 4) is a SSTR4 agonist.
    SSTR4 agonist-1 tartrate
  • HY-157303
    SSTR5 antagonist 3
    		Antagonist
    SSTR5 antagonist 3 (Compound 23) is an orally active somatostatin receptor subtype 5 (SSTR5) antagonist with low hERG inhibition. SSTR5 antagonist 3 exhibits potency with IC50 values of 2.8 nM and 1.4 nM in human and mouse, respectively. SSTR5 antagonist 3 can be used for the research of anti-gallstone.
    SSTR5 antagonist 3
  • HY-P1207
    BIM 23052
    		Agonist
    BIM 23052 is a somatostatin receptor 5 agonist. BIM 23052 can induce gastric emptying.
    BIM 23052
Cat. No. Product Name / Synonyms Application Reactivity
Somatostatin Receptor Isoform Comparison

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